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US 9,670,229 B2Granted
5-HT3 receptor antagonists
AssigneeTakeda Pharmaceutical Company Limited
InventorsStephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Shota Kikuchi, Todd Macklin, Maria Hopkins
Life of this patent
Estimating the term…
Abstract
The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Claims11
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof or N-oxide thereof, wherein:
- Z is O or NRa, wherein is hydrogen or C1-6 alkyl;
- R1 is a ring of the formula (a)-(h) below:
- R2 is hydrogen, C1-6 alkyl, or C1-6 haloalkyl;
- each R3 is independently hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkoxy, or halo, and can be present on any carbon atom in the rings;
- R4 is pyridinyl or pyrazolyl, each optionally substituted with one or two substituents independently selected from C1-6 alkyl, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 alkoxy, cyano, and halo;
- X1, X2, X3, and X4 are each CR5;
- each R5 is independently hydrogen, C1-6 alkyl, halo, hydroxy, or cyano, provided that at least one of R5 is hydrogen;
- and
- X5 is N.
7 more elements
Dependencies are inferred from the claim text.